Other

Indena S.p.a.

Vivacell Biotechnology Espana, S.l.

Deutsches Institut Fuer Ernaehrungsforschung Potsdam-rehbruecke

Deutsches Institut Für Ernahrungsforschung Potsdam-rehbrücke

Deutsches Institut Fuer Ernaehrungsforschung

Emerald Health Pharmaceuticals Inc.

Giovanni Appendino

Wolfgang Meyerhof

Maik Behrens

Anne Brockhoff

Christina Kuhn

Eduardo Muñoz Blanco

María Luz Bellido Cabello De Alba

Eduardo Munoz Blanco

Maria Luz Bellido Cabello De Alba

Paolo Morazzoni

Gabriele Fontana

Antonella Riva

Vincenzo Di Marzo

Alberto Minassi

Alberto Pagani

Valeria D'Auria

Paolo Indena SpA Morazzoni

Antonella Indena SpA Riva

Gabriele Indena SpA Fontana

Triterpenoid derivatives and compositions comprising said triterpenoids derivatives of Formula (I) are described, wherein R&#x2550;&#x2014;C(O)NHOH. Said triterpenoids and compositions show capacity to bind PHD2, stabilize HIF-1&#x3b1; and HIF-2&#x3b1; proteins, activate the HIF pathway in different cell types, induce angiogenesis in human endothelial vascular cell, show neuroprotective activity in vitro and in vivo, antidiabetic activity and reduce the levels of lipids in vivo, and increase the plasma levels of Erythropoietin in vivo. The triterpenoid derivatives described act also in a selective manner and do not induce Nrf2 activation, NF-&#x3ba;B inhibition, STAT3 inhibition, and TGR5 activation, which are known activities of the natural triterpenoid precursors. Said triterpenoid derivatives are useful in the treatment of conditions and diseases which are responsive to HIF activation such as stroke, cerebral palsy, traumatic injuries and neurodegenerative diseases; and also IBD, myocardial ischaemia-reperfusion injury, acute lung injury, diabetic and chronic wounds, organ transplantation, acute kidney injury or arterial diseases. 

Hydroxamate triterpenoid derivatives

The present invention relates to novel cannabigerol quinone derivatives of formula (I) wherein R is the carbon atom of a linear or branched group, represented by: aryl, alkenyl, alkynyl or alcoxycarbonil groups; or wherein R is the nitrogen atom of a linear or branched group, represented by: alkylamino, arylamino, alkenylamino or alkynylamino groups; or, alternatively, R represents a bond between 2 molecules of formula (I) forming a dimer. The invention also relates to the use of any of the compounds of formula (I) as medicaments in therapy, particularly for treating PPARg-related diseases due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds. 

Cannabigerol derivatives

The present invention relates to novel cannabidiol quinone derivatives of formula (I) (I) wherein R is the carbon atom of a, linear or branched group, represented by: alkyl, aryl, alkenyl, alkynyl, acyl or alkoxycarbonyl groups; or wherein R is the nitrogen atom of a, linear or branched group represented by: alkylamine, arylamine, alkenylamine or alkynylamine groups. The invention also relates to the use of any of the compounds of formula (I) as medicaments in therapy, particularly for treating diseases and conditions responsive to PPARg modulation due to their high PPARg agonistic effect lacking electrophilic (Nrf2 activation) and cytotoxic activities. This invention also provides pharmaceutical compositions comprising said compounds and method of treating diseases with said compounds. 

Cannabidiol quinone derivatives

The present invention relates to a new method for isolating ingenol (CHO) from mixtures of diterpenoid esters and ingenol esters in a single step. Ingenol isolated by means of this method can be used as a precursor for the synthesis of biologically active ingenol derivatives, such as ingenol-3-angelate and ingenol-3-tigliate.

Method of isolating ingenol

Cannabinoid quinone derivatives. The present invention refers to cannabinoid quinone derivatives to be used as medicaments, particularly as PPAR gamma (PPARg) agonists for treating diseases which etiology is based on an impaired PPARg function as transcription factor i.e. PPARg-related diseases.

Cannabinoid quinone derivatives

The present invention relates to antagonists and agonists of the human bitter-taste receptors hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and hTAS2R47. The invention also relates to methods for identifying further molecules that suppress or enhance bitter taste transduction or bitter taste response mediated by hTAS2R40, hTAS2R43, hTAS2R44, hTAS2R46, and/or hTAS2R47 and uses thereof.

Methods of identifying antagonists of the hTAS2R46 bitter taste receptor

The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.

Agonists of bitter taste receptors and uses thereof

The present invention relates to agonists of the human bitter-taste receptors hTAS2R46, hTAS2R47 and hTAS2R50 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R46, hTAS2R47 and hTAS2R50 bitter taste transduction or bitter taste response.

Methods of identifying agonists and antagonists of hTASR bitter taste receptors

The compounds of the general formula (I) in which X is represents two hydrogen atoms, a &#x3c0;-bond, oxygen or methylene: R2 is a C-Caryl, or arylalkyl residue: R3 is hydrogen, 2-hydroxyethyl or 2-aminoethyl are useful for the treatment of pathologies mediated by vanilloid receptors type I. 

Growing community of inventors

Turin, Italy

Giovanni Appendino